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Synthesis and biological evaluation of fluoro-substituted spiro-isoxazolines as potential anti-viral and anti-cancer agents.

Authors :
Das P
Boone S
Mitra D
Turner L
Tandon R
Raucher D
Hamme AT 2nd
Source :
RSC advances [RSC Adv] 2020 Aug 17; Vol. 10 (50), pp. 30223-30237. Date of Electronic Publication: 2020 Aug 17 (Print Publication: 2020).
Publication Year :
2020

Abstract

Electrophilic fluorine-mediated dearomative spirocyclization has been developed to synthesize a range of fluoro-substituted spiro-isoxazoline ethers and lactones. The in vitro biological assays of synthesized compounds were probed for anti-viral activity against human cytomegalovirus (HCMV) and cytotoxicity against glioblastomas (GBM6) and triple negative breast cancer (MDA MB 231). Interestingly, compounds 4d and 4n showed significant activity against HCMV (IC <subscript>50</subscript> ∼ 10 μM), while 4l and 5f revealed the highest cytotoxicity with IC <subscript>50</subscript> = 36 to 80 μM. The synthetic efficacy and biological relevance offer an opportunity to further drug-discovery development of fluoro-spiro-isoxazolines as novel anti-viral and anti-cancer agents.<br />Competing Interests: There are no conflicts to declare.<br /> (This journal is © The Royal Society of Chemistry.)

Details

Language :
English
ISSN :
2046-2069
Volume :
10
Issue :
50
Database :
MEDLINE
Journal :
RSC advances
Publication Type :
Academic Journal
Accession number :
35518245
Full Text :
https://doi.org/10.1039/d0ra06148d